WO2005111064A8 - Cyclopeptide derivatives with anti-integrin activity - Google Patents

Cyclopeptide derivatives with anti-integrin activity

Info

Publication number
WO2005111064A8
WO2005111064A8 PCT/IT2005/000262 IT2005000262W WO2005111064A8 WO 2005111064 A8 WO2005111064 A8 WO 2005111064A8 IT 2005000262 W IT2005000262 W IT 2005000262W WO 2005111064 A8 WO2005111064 A8 WO 2005111064A8
Authority
WO
WIPO (PCT)
Prior art keywords
useful
compounds
inhibitors
integrin activity
cyclopeptide derivatives
Prior art date
Application number
PCT/IT2005/000262
Other languages
French (fr)
Other versions
WO2005111064A1 (en
Inventor
Pozzo Alma Dal
Sergio Penco
Giuseppe Giannini
Maria Ornella Tinti
Claudio Pisano
Loredana Vesci
Ming Hong Ni
Original Assignee
Sigma Tau Ind Farmaceuti
Pozzo Alma Dal
Sergio Penco
Giuseppe Giannini
Maria Ornella Tinti
Claudio Pisano
Loredana Vesci
Ming Hong Ni
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to JP2007512736A priority Critical patent/JP2008500971A/en
Priority to AU2005243418A priority patent/AU2005243418A1/en
Priority to MXPA06012887A priority patent/MXPA06012887A/en
Priority to SI200530986T priority patent/SI1751176T1/en
Priority to PL05742999T priority patent/PL1751176T3/en
Priority to DE602005019876T priority patent/DE602005019876D1/en
Priority to US11/596,190 priority patent/US20070178045A1/en
Priority to BRPI0510985-0A priority patent/BRPI0510985A/en
Application filed by Sigma Tau Ind Farmaceuti, Pozzo Alma Dal, Sergio Penco, Giuseppe Giannini, Maria Ornella Tinti, Claudio Pisano, Loredana Vesci, Ming Hong Ni filed Critical Sigma Tau Ind Farmaceuti
Priority to EP05742999A priority patent/EP1751176B1/en
Priority to AT05742999T priority patent/ATE460426T1/en
Priority to CA002562576A priority patent/CA2562576A1/en
Priority to DK05742999.5T priority patent/DK1751176T3/en
Priority to RSP-2010/0231A priority patent/RS51300B/en
Publication of WO2005111064A1 publication Critical patent/WO2005111064A1/en
Publication of WO2005111064A8 publication Critical patent/WO2005111064A8/en
Priority to CY20101100440T priority patent/CY1110039T1/en
Priority to HR20100301T priority patent/HRP20100301T1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/12—Cyclic peptides with only normal peptide bonds in the ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biotechnology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Formula (I) compounds are described c(R1-Arg- Gly-Asp-R2) where the meanings of the various groups are as described here below, which are integrin inhibitors, and particularly inhibitors of integrins of the αvβ3 and αvβ5 family, and therefore are useful as medicaments, particularly for the treatment of the diseases underlying abnormal angiogenesis, such as retinopathy, acute renal failure, osteoporosis and metastases. The compounds described herein, when suitably labelled, are also useful as diagnostic agents, especially for the detection of small tumor masses and arterial occlusion events, and as targeted drug vectors.
PCT/IT2005/000262 2004-05-13 2005-05-04 Cyclopeptide derivatives with anti-integrin activity WO2005111064A1 (en)

Priority Applications (15)

Application Number Priority Date Filing Date Title
EP05742999A EP1751176B1 (en) 2004-05-13 2005-05-04 Cyclopeptide derivatives with anti-integrin activity
AU2005243418A AU2005243418A1 (en) 2004-05-13 2005-05-04 Cyclopeptide derivatives with anti-integrin activity
AT05742999T ATE460426T1 (en) 2004-05-13 2005-05-04 CYCLOPEPTIDE DERIVATIVES WITH ANTI-INTEGRIN EFFECT
PL05742999T PL1751176T3 (en) 2004-05-13 2005-05-04 Cyclopeptide derivatives with anti-integrin activity
DE602005019876T DE602005019876D1 (en) 2004-05-13 2005-05-04 CYCLOPEPTIDE DERIVATIVES WITH ANTI-INTEGRIN EFFECT
US11/596,190 US20070178045A1 (en) 2004-05-13 2005-05-04 Cyclopeptide derivatives with anti-integrin activity
BRPI0510985-0A BRPI0510985A (en) 2004-05-13 2005-05-04 cyclopeptide derivatives with activity against integrin
JP2007512736A JP2008500971A (en) 2004-05-13 2005-05-04 Cyclopeptide derivatives having anti-integrin activity
MXPA06012887A MXPA06012887A (en) 2004-05-13 2005-05-04 Cyclopeptide derivatives with anti-integrin activity.
SI200530986T SI1751176T1 (en) 2004-05-13 2005-05-04 Cyclopeptide derivatives with anti-integrin activity
CA002562576A CA2562576A1 (en) 2004-05-13 2005-05-04 Cyclopeptide derivatives with anti-integrin activity
DK05742999.5T DK1751176T3 (en) 2004-05-13 2005-05-04 Cyclopeptide derivatives with anti-integrin activity
RSP-2010/0231A RS51300B (en) 2004-05-13 2005-05-04 Cyclopeptide derivatives with anti-integrin activity
CY20101100440T CY1110039T1 (en) 2004-05-13 2010-05-19 CYCLOPEPTIDE DERIVATIVES WITH ANTI-INTEGRIN ACTIVITY
HR20100301T HRP20100301T1 (en) 2004-05-13 2010-05-27 Cyclopeptide derivatives with anti-integrin activity

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITRM2004A000239 2004-05-13
IT000239A ITRM20040239A1 (en) 2004-05-13 2004-05-13 CYCLOPEPTIDIC DERIVATIVES FOR ANTI-INTEGRINE ACTIVITIES.

Publications (2)

Publication Number Publication Date
WO2005111064A1 WO2005111064A1 (en) 2005-11-24
WO2005111064A8 true WO2005111064A8 (en) 2006-02-09

Family

ID=34968013

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IT2005/000262 WO2005111064A1 (en) 2004-05-13 2005-05-04 Cyclopeptide derivatives with anti-integrin activity

Country Status (23)

Country Link
US (1) US20070178045A1 (en)
EP (1) EP1751176B1 (en)
JP (1) JP2008500971A (en)
KR (1) KR20070012524A (en)
CN (1) CN1953990A (en)
AR (1) AR048957A1 (en)
AT (1) ATE460426T1 (en)
AU (1) AU2005243418A1 (en)
BR (1) BRPI0510985A (en)
CA (1) CA2562576A1 (en)
CY (1) CY1110039T1 (en)
DE (1) DE602005019876D1 (en)
DK (1) DK1751176T3 (en)
ES (1) ES2340862T3 (en)
HR (1) HRP20100301T1 (en)
IT (1) ITRM20040239A1 (en)
MX (1) MXPA06012887A (en)
PL (1) PL1751176T3 (en)
PT (1) PT1751176E (en)
RS (1) RS51300B (en)
SI (1) SI1751176T1 (en)
TW (1) TW200606178A (en)
WO (1) WO2005111064A1 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI426905B (en) * 2006-02-09 2014-02-21 Enzon Pharmaceuticals Inc Multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin for treatment of breast, colorectal, pancreatic, ovarian and lung cancers
EP1961759A1 (en) * 2007-02-21 2008-08-27 Universita'degli Studi Di Milano Integrin targeted cyclopeptide ligands, their preparation and use
TWI474819B (en) 2012-05-15 2015-03-01 Univ Nat Cheng Kung Regulator and pharmaceutical composition encompassing the regulator
EA201591806A1 (en) * 2013-03-15 2016-01-29 Байоджен Ма Инк. TREATMENT AND PREVENTION OF ACUTE RENAL FAILURE WITH THE USE OF ANTI-ALPHA-V-BETA-5 ANTIBODIES
CN103588863B (en) * 2013-11-15 2016-08-17 苏州强耀生物科技有限公司 RGD cyclic peptide synthesis and preparation process
WO2022183360A1 (en) * 2021-03-02 2022-09-09 Tsao Yeou Ping Short synthetic peptide and their uses for treating dry eye disease

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4310643A1 (en) * 1993-04-01 1994-10-06 Merck Patent Gmbh Cyclic adhesion inhibitors
US5449761A (en) * 1993-09-28 1995-09-12 Cytogen Corporation Metal-binding targeted polypeptide constructs
US6027711A (en) * 1995-06-07 2000-02-22 Rhomed Incorporated Structurally determined metallo-constructs and applications
DE19725368A1 (en) * 1997-06-16 1998-12-17 Merck Patent Gmbh New cyclic peptides inhibit ligand binding to integrins
ITRM20040242A1 (en) * 2004-05-13 2004-08-13 Ist Naz Stud Cura Dei Tumori "7-T-BUTOSSIIMMINOMETILCAMPTOTECINA CONJUGED IN POSITION 20 WITH INTEGRINE ANTAGONISTS.
ITRM20040240A1 (en) * 2004-05-13 2004-08-13 Ist Naz Stud Cura Dei Tumori CAMPTOTECINE CONJUGATED IN POSITION 7 WITH INTEGRINE ANTAGONISTS.

Also Published As

Publication number Publication date
CN1953990A (en) 2007-04-25
JP2008500971A (en) 2008-01-17
ITRM20040239A1 (en) 2004-08-13
EP1751176B1 (en) 2010-03-10
AU2005243418A1 (en) 2005-11-24
SI1751176T1 (en) 2010-06-30
KR20070012524A (en) 2007-01-25
MXPA06012887A (en) 2007-02-15
CA2562576A1 (en) 2005-11-24
HRP20100301T1 (en) 2010-06-30
TW200606178A (en) 2006-02-16
ATE460426T1 (en) 2010-03-15
RS51300B (en) 2010-12-31
DK1751176T3 (en) 2010-06-14
CY1110039T1 (en) 2012-05-23
DE602005019876D1 (en) 2010-04-22
EP1751176A1 (en) 2007-02-14
PL1751176T3 (en) 2010-08-31
PT1751176E (en) 2010-05-12
BRPI0510985A (en) 2007-12-04
US20070178045A1 (en) 2007-08-02
AR048957A1 (en) 2006-06-14
ES2340862T3 (en) 2010-06-10
WO2005111064A1 (en) 2005-11-24

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